Development of Novel Indole-3-Aldehyde–Loaded Gastro-Resistant Spray-Dried Microparticles for Postbiotic Small Intestine Local Delivery

喷雾干燥 乙基纤维素 乙醇 化学 原材料 纤维素 微粒 色谱法 溶剂 食品科学 化学工程 有机化学 工程类 聚合物
作者
Matteo Puccetti,Stefano Giovagnoli,Teresa Zelante,Luigina Romani,Maurizio Ricci
出处
期刊:Journal of Pharmaceutical Sciences [Elsevier BV]
卷期号:107 (9): 2341-2353 被引量:44
标识
DOI:10.1016/j.xphs.2018.04.023
摘要

Considering the recent evidence on the therapeutic potential of postbiotics, this study focused on 2 main goals: (1) to develop an enteric microparticle (MP) formulation for intestinal localized delivery of indole-3-aldehyde (3-IAld) (a microbial-derived metabolite produced by the host's lactobacilli during the catabolic pathway of tryptophan) and (2) to provide support in the employment of spray-drying as innovative one-step manufacturing technique for enteric products. For this purpose, special attention was taken in the knowledge of the influence of equipment setup and feedstock properties on MP enteric behavior. Eudragit® S100 and L100 and ethyl cellulose were used as wall materials and NaOH and ethanol solutions as solvent systems. 3-IAld loading was maintained at 10% w/w. As postulated, feedstock properties influenced spray-drying regime. In addition, they prevailed over other spray-drying process factors in determining MP enteric behavior. Albeit the high buckling regime that produced crumped particles, gastro resistance was obtained by spray-drying 2:1 Eudragit® S100:L100 with 30% w/w ethyl cellulose in ethanol solution. These results support the use of spray-drying as a method for manufacturing gastro-resistant MP. The obtained 3-IAld–loaded enteric MP will be useful to investigate novel postbiotic-based treatments in different therapeutic areas.
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